Sulfasalazine-native (Sulfasalazin-nativ)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceSulfasalazineSulfasalazine
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    ATOLL, LLC     Russia
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    NATIVA, LLC     Russia
    • Dosage form: & nbspfilm coated tablets
    Composition:

    Composition for 1 tablet, film-coated:

    Component name

    Amount, mg

    Active substance:


    Sulfasalazine

    500,0

    Excipients:


    Crospovidone

    35,0

    Pregelatinized starch

    89,7

    Silica colloidal dioxide

    3,3

    Magnesium stearate

    12,0

    Composition of the film shell:


    Film sheath

    (polyvinyl alcohol - 40.00%, talcum - 14.80%, macrogol 3350 - 20.20%, titanium dioxide - 21.65%, iron coloring agent, yellow oxide -3.35%)

    6,0
    Description:

    Round, biconvex tablets with bevelled edges, covered with a film coating of yellow color. On the fracture, the core is brownish-yellow, inclusions are allowed.

    Pharmacotherapeutic group:Antimicrobial and anti-inflammatory intestinal
    ATX: & nbsp

    J.04.A.A   Aminosalicylic acid and its derivatives

    Pharmacodynamics:

    Sulfasalazine selectively accumulates in the connective tissue of the intestine with the release of 5-aminosalicylic acid (5-ASA), which has anti-inflammatory activity, and sulfapyridine, which possesses antimicrobial bacteriostatic activity.

    Pharmacokinetics:

    Suction

    About 30% of the sulfasalazine contained in the film-coated tablets are absorbed from the small intestine, the remaining 70% are digested with the intestinal microflora to form sulfapyridine 60 - 80% and 25% - 5-ASA.

    Distribution

    There are large individual differences in the maximum serum concentrations (CmOh) sulfasalazine and its metabolites; in "slow acetylators" they are higher, which increases the risk of unwanted effects. Sulfasalazine reaches its maximum concentration 3 to 12 hours after taking the tablets coated with a film coat.

    Linkage with plasma proteins of sulfasalazine - 99%, sulfapyridine - 50%, 5-ASA - 43%.

    Metabolism

    Sulfapyridine is metabolized in the liver by hydroxylation with the formation of inactive metabolites, 5-ASA - by acetylation.

    Excretion

    Half-life (T1/2) sulfasalazine - 5 - 10 hours, sulfapiridine - 6 - 14 hours, 5-ASA - 0,6 - 1,4 hours.

    The intestine removes 5% sulfapiridine and 67% 5-ASA, kidneys - 75 - 91% sucked sulphasalazine (for 3 days).

    Indications:

    - Ulcerative colitis (treatment of exacerbations and maintenance therapy in the phase of remission);

    - Crohn's disease (mild and moderate forms in the phase of exacerbation);

    - rheumatoid arthritis; juvenile rheumatoid arthritis with ineffectiveness of non-steroidal anti-inflammatory drugs (NSAIDs).

    Contraindications:

    - Hypersensitivity to sulfasalazine or other components of the drug, as well as sulfonamides or salicylates;

    - porphyria;

    - granulocytopenia;

    - Aplastic anemia;

    - congenital deficiency of glucose-6-phosphate dehydrogenase (risk of jaundice development);

    - Hepatic and / or renal insufficiency;

    - children under 10 years of age and / or body weight of 35 kg or less, with chronic inflammatory bowel disease (for this dosage form and dosage);

    - Obstruction of the intestines or urinary tract;

    - Children under 6 years of age with juvenile rheumatoid arthritis (efficacy and safety not established);

    lactation period.

    Carefully:

    Bronchial asthma, atopic dermatitis, allergic reactions in the anamnesis (there may be cross-allergic reactions to furosemide, thiazide diuretics, sulfonylurea derivatives, inhibitors of carbonic anhydrase),systemic forms of juvenile rheumatoid arthritis (risk of developing serum sickness); pregnancy.

    Pregnancy and lactation:

    During pregnancy, prescription of the drug is possible only on strict indications and in a minimally effective dose. If the course of the disease allows, then in the last trimester of pregnancy, the drug should be stopped (sulfasalazine displaces bilirubin from the bond with plasma proteins, thereby increasing the risk of developing nuclear jaundice and hyperbilirubinemia in newborns - toxic damage to the nerve centers of the brain). In newborns with deficiency of glucose-6-phosphate dehydrogenase, the development of hemolytic anemia is possible.

    Sulfasalazine is normally secreted into breast milk in very small quantities, but the risk of developing nuclear jaundice in preterm infants and in high-risk children is also increasing. The concentration of sulfapiridine in mother's milk is 40% of the concentrations in the mother's plasma. If it is necessary to administer the drug Sulfasalazine-native during lactation breastfeeding should be discontinued.

    Dosing and Administration:

    Inside, after eating.

    Ulcerative colitis, Crohn's disease:

    Adults and children over 16 years of age: in the first day of 500 mg 4 times a day; on the second day, 1 g 4 times a day; in the third and subsequent days of 1.5 - 2 g 4 times a day. After the acute clinical symptoms of ulcerative colitis subsided adults and adolescents and / or with a body weight of more than 65 kg prescribe a maintenance dose of 500 mg 3 - 4 times a day for several months.

    Children from 10 years to 16 years and / or body weight from 35 kg to 50 kg: 500 mg 4 times a day.

    Supportive therapy for children and adolescents under 16 years of age and / or body weight less than 65 kg Not recommended.

    The maximum daily intake for adults - 8 g, for children under 16 years - 2 g.

    Rheumatoid arthritis and juvenile rheumatoid arthritis

    Adults and children over 16 years of age: during the first week, 500 mg once a day, 500 mg twice a day for the second, 500 mg 3 times a day for the third, and so on. The therapeutic dose can be from 1.5 g to 3 g per day. The clinical effect appears after 6-10 weeks of therapy. The course of treatment is 6 months or more.

    Children from 6 to 8 years and / or body weight of 20-29 kg: 1 tablet 2 times a day.

    Children from 8 to 12 years of age and / or body weight of 20-39 kg: 1 tablet 2-3 times a day.

    Children from 12 to 16 years of age and / or body weight of 40-50 kg: 1 tablet 3 times a day or 2 tablets 2 times a day.

    Children over 16 years of age and / or body weight over 50 kg: 2 pills 2 times a day. The maximum daily dose for children is 2 g or 40 - 50 mg / kg body weight.
    Side effects:

    Side effects are associated with the degree of plasma concentration of sulfapyridine, especially in people with slow acetylation. More often, side effects are observed in patients with rheumatoid arthritis.

    Impaired nervous system: headache, peripheral neuropathy, dizziness, convulsions, ataxia, aseptic meningitis.

    Disorders of the psyche: hallucinations, sleep disturbance, depression.

    Disorders from the gastrointestinal tract: nausea, vomiting, diarrhea, decreased appetite, pancreatitis, stomatitis, abdominal pain.

    Disorders from the liver and bile ducts: drug hepatitis.

    Violations from the blood and lymphatic system: macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia due to enzyme disturbances - in unstable hemoglobin molecules (calf Heinz-Ehrlich), methemoglobinemia, agranulocytosis, thrombocytopenia, aplastic anemia, hypoprothrombinemia.

    Disorders from the kidneys and urinary tract: proteinuria, hematuria, crystalluria, nephrotic syndrome.

    Violations of the genitals and breast: Transient oligospermia and male infertility.

    Disturbances from the respiratory system, chest and mediastinal organs: shortness of breath, cough, interstitial pneumonitis, fibrosing alveolitis, infiltrates in the lung tissue.

    Hearing disorders and labyrinthine disturbances: noise in ears.

    Laboratory and instrumental data: hyperbilirubinemia, increased activity of alkaline phosphatase, hepatic transaminases.

    Immune system disorders: generalized skin rash, urticaria, erythema, pruritus, exfoliative dermatitis, photosensitivity, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), fever, lymphadenopathy, serum sickness, periorbital edema, eosinophilia, periarteritis nodosa, anaphylactic shock.

    General disorders and disorders at the site of administration: hyperthermia, parotitis, possibly staining urine, skin or soft contact lenses in a yellow-orange color.

    Overdose:

    Symptoms: nausea, vomiting, abdominal pain, dizziness. When very high doses are used, there may be: anuria, crystalluria, hematuria, symptoms toxic damage of the central nervous system (convulsions). Treatment: symptomatic. It is necessary to provoke vomiting, rinse the stomach, intestines; urine alkalinization, forced diuresis. In anuria and / or renal failure, fluid and electrolyte intake should be limited.

    Interaction:

    Sulfasalazine reduces the absorption of folic acid and digoxin.

    Strengthens the effect of anticoagulants, antiepileptic and oral hypoglycemic agents, as well as side effects of cytostatics, immunosuppressants, hepato- and nephrotoxic agents.

    Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression. Antibacterial agents, in connection with the oppressive effect on the intestinal flora, reduce the effectiveness of sulfasalazine in ulcerative colitis.
    Special instructions:

    During the period of treatment, a general blood test is recommended (at the beginning of therapy: 1-2 times a month, then every 3-6 months of treatment) and urinalysis (with renal failure),periodic activity control "hepatic" enzymes in the blood plasma, the use of increased amounts of fluid. Sulfasalazine it is recommended with caution that patients with systemic forms of juvenile rheumatoid arthritis should be prescribed. there is a risk of unwanted effects, incl. serum sickness (fever, nausea, vomiting, headache, skin rash, impaired liver function).

    Effect on the ability to drive transp. cf. and fur:

    Care must be taken when driving vehicles and mechanisms due to the possibility of dizziness.

    Form release / dosage:

    Tablets, film-coated 500 mg.

    Packaging:

    For 50 tablets in bottles of polyethylene terephthalate, sealed with high density polyethylene caps.

    One bottle together with the instruction for use is placed in a cardboard box.
    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004196
    Date of registration:16.03.2017
    Expiration Date:16.03.2022
    The owner of the registration certificate:NATIVA, LLC NATIVA, LLC Russia
    Manufacturer: & nbsp
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